In Vitro-ln Vivo Correlation for Modified-Release Formulations

Drewe, Jürgen; Guitard, P

doi:10.1002/jps.2600820204

Cited by 31 publications

(18 citation statements)

References 11 publications

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“…Level B correlation applies the principles of statistical moment analysis. It compares the mean in vitro dissolution time to either the mean residence time or the mean in vivo dissolution time (77,78), so it does not reflect the actual in vivo plasma concentration curve. Therefore, level B correlation alone cannot support biowaivers.…”

Section: In Vitro and In Vivo Relationships And Bioequivalence Challementioning

confidence: 99%

The Science of USP 1 and 2 Dissolution: Present Challenges and Future Relevance

Gray¹,

et al. 2009

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Since its inception, the dissolution test has come under increasing levels of scrutiny regarding its relevance, especially to the correlation of results to levels of drug in blood. The technique is discussed, limited to solid oral dosage forms, beginning with the scientific origins of the dissolution test, followed by a discussion of the roles of dissolution in product development, consistent batch manufacture (QC release), and stability testing. The ultimate role of dissolution testing, "to have the results correlated to in vivo results or in vivo in vitro correlation," is reviewed. The recent debate on mechanical calibration versus performance testing using USP calibrator tablets is presented, followed by a discussion of variability and hydrodynamics of USP Apparatus 1 and Apparatus 2. Finally, the future of dissolution testing is discussed in terms of new initiatives in the industry such as quality by design (QbD), process analytical technology (PAT), and design of experiments (DOE).

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Section: In Vitro and In Vivo Relationships And Bioequivalence Challementioning

confidence: 99%

The Science of USP 1 and 2 Dissolution: Present Challenges and Future Relevance

Gray¹,

et al. 2009

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“…the Levy plot (Levy et al, 1965), is nonlinear. While in most cases a linear time transformation proved sufficient (Brockmeier et al, 1985;Schliecker et al, 2004;Nishimura et al, 2007;Jantratid et al, 2009;Cardot and Davit, 2012), several reports have found that / is a convex function, i.e., the Levy plot shows an upward curvature (Drewe and Guitard, 1993;Humbert et al, 1994;Hemmingsen et al, 2011;Cardot and Davit, 2012;Kakhi et al, 2013;Klancar et al, 2013). It will be shown in this study that this means that dissolution is decelerated in vivo (a < 1), or respectively, accelerated in vitro, and that the Levy plot can be described by a power function.…”

Section: Introductionmentioning

confidence: 79%

Modeling accelerated and decelerated drug release in terms of fractional release rate

Weiß

2015

European Journal of Pharmaceutical Sciences

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“…We suggest that this flip flop-like phenomenon could be present at k el /k a ratios smaller than 1 (i.e., 0.2). Absorption is recognized as the rate-limiting step for BCS class III drug formulations (54,55); however, for the metformin formulation, test formulations with faster release (Fig. 4, smaller t 50 and larger n) than the reference formulation generated plasma profiles with higher C max and AUC, resulting in declaration of nonbioequivalence.…”

Section: Discussionmentioning

confidence: 99%

“…MDT and MRT (40,54) were not useful to discriminate between nonbioequivalent and bioequivalent formulations nor to set dissolution specifications ( Fig. 8 and S17, S18, and S25) highlighting the complex composition of the multidimensional BE space.…”

Section: Discussionmentioning

confidence: 99%

Statistical Comparison of Dissolution Profiles to Predict the Bioequivalence of Extended Release Formulations

Gómez-Mantilla

Schaefer

Casabó

et al. 2014

AAPS J

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Abstract. Appropriate setting of dissolution specification of extended release (ER) formulations should include precise definition of a multidimensional space of complex definition and interpretation, including limits in dissolution parameters, lag time (t-lag), variability, and goodness of fit. This study aimed to set dissolution specifications of ER by developing drug-specific dissolution profile comparison tests (DPC tests) that are able to detect differences in release profiles between ER formulations that represent a lack of bioequivalence (BE). Dissolution profiles of test formulations were simulated using the Weibull and Hill models. Differential equations based in vivo-in vitro correlation (IVIVC) models were used to simulate plasma concentrations. BE trial simulations were employed to find the formulations likely to be declared bioequivalent and nonbioequivalent (BE space). Customization of DPC tests was made by adjusting the delta of a recently described tolerated difference test (TDT) or the limits of rejection of f2. Drug k a (especially if k a is small), formulation lag time (t-lag), the number of subjects included in the BE studies, and the number of sampled time points in the DPC test were the factors that affected the most these setups of dissolution specifications. Another recently described DPC test, permutation test (PT), showed excellent statistical power. All the formulations declared as similar with PT were also bioequivalent. Similar case-specific studies may support the biowaiving of ER drug formulations based on customized DPC tests.

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In Vitro-ln Vivo Correlation for Modified-Release Formulations

Cited by 31 publications

References 11 publications

The Science of USP 1 and 2 Dissolution: Present Challenges and Future Relevance

The Science of USP 1 and 2 Dissolution: Present Challenges and Future Relevance

Modeling accelerated and decelerated drug release in terms of fractional release rate

Statistical Comparison of Dissolution Profiles to Predict the Bioequivalence of Extended Release Formulations

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